Isradipine and lacidipine: effects in vivo and in vitro on Trypanosoma cruzi epimastigotes.
1. Isradipine and lacidipine, two new drugs that are members of the nitro-aryl-1,4-dihydropyridine family, produced inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. 2. Isradipine was found to be the most potent derivative in both, in growth cultures (I50 = 20.8 microM) and in vivo oxygen uptake (I50 = 31.1 microM). 3. Diltiazem and verapamil, two well-known calcium channel antagonists, lacked inhibitory activity, even at a 100 microM concentration. 4. The present findings indicate that the trypanocide effects exerted by isradipine and lacidipine are not related with a disruption of the calcium homeostasis of the parasite.
Núñez-Vergara
L J
LJ
Facultad De Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago, Chile.
Squella
J A
JA
Bollo-Dragnic
S
S
Marín-Catalán
R
R
Pino
L
L
Díaz-Araya
G
G
Letelier
M E
ME
D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002417:Cattle; D004095:Dihydropyridines / Q000494:pharmacology*; D004110:Diltiazem / Q000494:pharmacology; D017275:Isradipine / Q000494:pharmacology*; D010101:Oxygen Consumption / Q000187:drug effects; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development; D014700:Verapamil / Q000494:pharmacology
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D014344:Trypanocidal Agents; C060285:lacidipine; D014700:Verapamil; D004110:Diltiazem; D017275:Isradipine